Albiglutide Fragment

Catalog No.S3734

For research use only.

Albiglutide fragment is one copy of a 30-amino-acid sequence of modified human GLP-1 (fragment 7-36).

Albiglutide Fragment Chemical Structure

CAS No. 782500-75-8

Purity & Quality Control

Choose Selective Glucagon Receptor Inhibitors

Biological Activity

Description Albiglutide fragment is one copy of a 30-amino-acid sequence of modified human GLP-1 (fragment 7-36).
In vitro

Albiglutide is a recombinant fusion protein consisting of two copies of a 30-amino-acid sequence of modified human GLP-1 (fragment 7-36), modified with a glycine substituted for the naturally occurring alanine at position 8 in order to augment resistance to DPP-4[1].

In vivo

Glucose lowering occurs within 24 h after a single dose of albiglutide, as a result of binding of the molecule to the GLP-1 receptor. The reduction in both fasting and postprandial glucose levels is dose related. Albiglutide is less potent than GLP-1. In animal models of diabetes, albiglutide administration stimulates increased β-cell mass. Following SC administration of a single 30-mg dose to patients with type 2 diabetes, maximum concentration is reached in 3-5 days with half-life of 3.6-6.8 days. The apparent volume of distribution after a single dose of albiglutide was 8.2-18.5 L. The eventual fate of albiglutide in the circulation is degradation into small peptides and individual amino acids. Albiglutide had no apparent effects on cardiovascular function, heart rate, electrocardiographic intervals, or respiratory function and did not produce any evidence of electrocardiographic abnormalities or arrhythmias in male cynomolgus monkeys. Furthermore, there were no albiglutide-related effects on neurobehavioral functional assessments. Albiglutide does not cross the blood–brain barrier to reach the satiety centers[1]. Albiglutide reduced myocardial infarct size and improved cardiac function and energetics following myocardial I/R injury which are associated with enhanced myocardial glucose uptake and a shift toward a more energetically favorable substrate metabolism by increasing both glucose and lactate oxidation[2].

Protocol (from reference)

Animal Research:

[2]

  • Animal Models: Male Sprague-Dawley rats
  • Dosages: 1, 3 or 10 mg/kg/day
  • Administration: s.c.
  • (Only for Reference)

Solubility (25°C)

In vitro

Water 100 mg/mL
(30.45 mM)


* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 3283.6
Formula

C148H224N40O45

CAS No. 782500-75-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC(C)C(C(=O)NC(C)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NCC(=O)NC(CCCNC(=N)N)C(=O)N)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CCC(=O)O)NC(=O)C(CCCCN)NC(=O)C(C)NC(=O)C(C)NC(=O)C(CCC(=O)N)NC(=O)CNC(=O)C(CCC(=O)O)NC(=O)C(CC(C)C)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(CO)NC(=O)C(CO)NC(=O)C(C(C)C)NC(=O)C(CC(=O)O)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C(CC5=CC=CC=C5)NC(=O)C(C(C)O)NC(=O)CNC(=O)C(CCC(=O)O)NC(=O)CNC(=O)C(CC6=CN=CN6)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03015519 Withdrawn Drug: Albiglutide|Drug: Placebo Diabetes Mellitus Type 2 GlaxoSmithKline August 14 2017 Phase 3
NCT02750930 Terminated Drug: Albiglutide|Device: Auto-injector Diabetes Mellitus Type 2 GlaxoSmithKline October 7 2016 Phase 4
NCT02229227 Completed Drug: Albiglutide|Drug: Insulin Glargine and Insulin Lispro Diabetes Mellitus Type 2 GlaxoSmithKline|PPD November 21 2014 Phase 3
NCT01475734 Completed Biological: albiglutide|Biological: placebo Diabetes Mellitus Type 2 GlaxoSmithKline December 2011 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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